Purpose of Glucuronidase Inhibitors?

[PuZo]

What is the purpose of glucuronidase inhibitors such as Calcium D-Saccharate Tetrahydrate? What role does it play in the body?

[neuron]

What is the purpose of glucuronidase inhibitors such as Calcium D-Saccharate Tetrahydrate? What role does it play in the body?

Calcium d-saccharate tetrahydrate is a gulcuronidase donor, not inhibitor.

An inhibitor would block phase II metabolism in the liver, which seeks to make substances more water soluble via conjugation (glucuronidation/sulfation).

If a drug is determined to be heavily dependent on phase II metabolism, then blocking this step would increase the drugs half-life.

[PuZo]

Calcium d-saccharate tetrahydrate is a gulcuronidase donor, not inhibitor.

An inhibitor would block phase II metabolism in the liver, which seeks to make substances more water soluble via conjugation (glucuronidation/sulfation).

If a drug is determined to be heavily dependent on phase II metabolism, then blocking this step would increase the drugs half-life.

So I'm assuming that would be the reason why it would be included?

[neuron]

So I'm assuming that would be the reason why it would be included?

I mispoke above. It is a glucuronidation donor, and a glucuronidase inhibitor. The end result is the same: decreased half-life of substances heavily dependent on phase II metabolism in the liver. It also blocks bacterial de-conjugation in the gut, which decreases biliary-intestinal re-circulation. The result of this process increases intestinal elimination of various substances.

OTOH, substances like quercetin or kaempferol decrease glucuronidation, and therefore would prolong the half-lives of substances undergoing phase II metabolism.

[PuZo]

I mispoke above. It is a glucuronidation donor, and a glucuronidase inhibitor. The end result is the same: decreased half-life of substances heavily dependent on phase II metabolism in the liver. It also blocks bacterial de-conjugation in the gut, which decreases biliary-intestinal re-circulation. The result of this process increases intestinal elimination of various substances.

OTOH, substances like quercetin or kaempferol decrease glucuronidation, and therefore would prolong the half-lives of substances undergoing phase II metabolism.

And quercetin has other benefits as well? Does the glucuronidase inhibition help regulate estrogen levels?

[neuron]

Does the glucuronidase inhibition help regulate estrogen levels?

One of the main ways through which the body regulates estrogen is via conjugation (phase II), and biliary excretion. Some % of that estrogen is de-conjugated (via bacterial beta-glucuronidase), and reabsorbed. Blocking this event with the previously mentioned substance does indeed lower systemic estrogen levels. The problem with this compound is that it can potentially decrease the half-lives of whatever else you are also supplementing with.

[PuZo]

One of the main ways through which the body regulates estrogen is via conjugation (phase II), and biliary excretion. Some % of that estrogen is de-conjugated (via bacterial beta-glucuronidase), and reabsorbed. Blocking this event with the previously mentioned substance does indeed lower systemic estrogen levels. The problem with this compound is that it can potentially decrease the half-lives of whatever else you are also supplementing with.

And the half life is once it's absorbed by the body? The other main substance would be DAA.

[TheWaffleIron]

And the half life is once it's absorbed by the body? The other main substance would be DAA.

Not quite.

http://en.wikipedia.org/wiki/Biological_half-life

The biological half-life or elimination half life of a substance is the time it takes for a substance (for example a metabolite, drug, signalling molecule, radioactive nuclide, or other substance) to lose half of its pharmacologic, physiologic, or radiologic activity... In a medical context, half-life may also describe the time it takes for the blood plasma concentration of a substance to halve ("plasma half-life") its steady-state.

[PuZo]

Not quite.

http://en.wikipedia.org/wiki/Biological_half-life

So it can decrease the total half life of the entire product?

[neuron]

And the half life is once it's absorbed by the body? The other main substance would be DAA.

After ingestion, it is absorbed via enterocytes and placed in the portal vein. It then circulates to the liver where the majority of metabolism (phase I/II) takes place (first pass).

You don't want to hear my thoughts on DAA.

[neuron]

So it can decrease the total half life of the entire product?

Anything predominantly metabolised by phase II metabolism.

This is mainly determined through urinalysis screening for conjugates vs. plasma metabolites.

[Adjusting]

After ingestion, it is absorbed via enterocytes and placed in the portal vein. It then circulates to the liver where the majority of metabolism (phase I/II) takes place (first pass).

You don't want to hear my thoughts on DAA.

I do. Spill it.

[PuZo]

i do. Spill it.

+1!

[BigPapiJR]

You don't want to hear my thoughts on DAA.

Let's hear it